6-Oxo and 6-thio purine analogs as antimycobacterial agents

6-Oxo and 6-thio analogs of purine were prepared based on the initial activity screening of a small, diverse purine library against Mycobacterium tuberculosis (Mtb). Certain 6-oxo and 6-thio-substituted purine analogs described herein showed moderate to good inhibitory activity. N9-substitution appa...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2013-04, Vol.21 (7), p.1685-1695
Main Authors: Pathak, Ashish K., Pathak, Vibha, Seitz, Lainne E., Suling, William J., Reynolds, Robert C.
Format: Article
Language:English
Subjects:
Animals
antibiotics
Antimycobacterial agents
Antitubercular Agents - chemistry
Antitubercular Agents - pharmacology
Antitubercular Agents - therapeutic use
Antitubercular Agents - toxicity
Cell Survival - drug effects
chemistry
Chlorocebus aethiops
Humans
Mice
Microbial Sensitivity Tests
Mycobacterium tuberculosis
Mycobacterium tuberculosis - drug effects
Purines
Purines - chemistry
Purines - pharmacology
Purines - therapeutic use
Purines - toxicity
screening
Sulfhydryl Compounds - chemistry
Sulfhydryl Compounds - pharmacology
Sulfhydryl Compounds - therapeutic use
Sulfhydryl Compounds - toxicity
Tuberculosis - drug therapy
Vero Cells
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Summary:6-Oxo and 6-thio analogs of purine were prepared based on the initial activity screening of a small, diverse purine library against Mycobacterium tuberculosis (Mtb). Certain 6-oxo and 6-thio-substituted purine analogs described herein showed moderate to good inhibitory activity. N9-substitution apparently enhances the anti-mycobacterial activity in the purine series described herein. Several 2-amino and 2-chloro purine analogs were also synthesized that showed moderate inhibitory activity against Mtb. 6-Oxo and 6-thio analogs of purine were prepared based on the initial activity screening of a small, diverse purine library against Mycobacterium tuberculosis (Mtb). Certain 6-oxo and 6-thio-substituted purine analogs described herein showed moderate to good inhibitory activity. N9-substitution apparently enhances the anti-mycobacterial activity in the purine series described herein. Several 2-amino and 2-chloro purine analogs were also synthesized that showed moderate inhibitory activity against Mtb.
ISSN:0968-0896
1464-3391
1464-3391
DOI:10.1016/j.bmc.2013.01.054